Generation of novel drug targeting protein kinase epsilon for type 2 diabetes mellitus.

Research Project

Project/Area Number	22710194
Research Category	Grant-in-Aid for Young Scientists (B)
Allocation Type	Single-year Grants
Research Field	Medical genome science
Research Institution	独立行政法人国立成育医療研究センター (2011) Tokai University (2010)
Principal Investigator	YONEZAWA Tomo 独立行政法人国立成育医療研究センター, システム発生・再生医学研究部, 流動研究員 (60515964)
Project Period (FY)	2010 – 2011
Project Status	Completed (Fiscal Year 2011)
Budget Amount *help	¥4,030,000 (Direct Cost: ¥3,100,000、Indirect Cost: ¥930,000) Fiscal Year 2011: ¥1,950,000 (Direct Cost: ¥1,500,000、Indirect Cost: ¥450,000) Fiscal Year 2010: ¥2,080,000 (Direct Cost: ¥1,600,000、Indirect Cost: ¥480,000)
Keywords	2型糖尿病 / プロテインキナーゼCε(PKCε) / 新規治療薬 / トランスレーショナルリサーチ / ゲノム / プロテインキナーゼC_ε / 既存薬X / 低分子化合物 / PKCε
Research Abstract	We identified the susceptible gene as a protein kinase C epsilon(PKCε) for type 2 diabetes mellitus via genome-wide association study using microsatellites, prompting us to generate the small molecule drug targeting PKCε. Our in silico strategy using over 60, 000 chemical library identified several potential compounds including drug X possibly affecting the activity of PKCε. We also validated the effect of them using molecular-and cell-based assay.